Skip to main content

3H-Tiotidine binding to guinea-pig cortical and striatal membranes

Abstract

3H-Tiotidine has been identified as a suitable radioligand for the H2-receptor (ref. 6). We have confirmed and extended structure-binding affinity studies in the guinea-pig cortex, and established a structure-binding affinity relationship consistent with the H2-receptor in guinea-pig striatum. Cimetidine-displaceable3H-tiotidine binding was observed also in the nucleus accumbens.

This is a preview of subscription content, access via your institution.

References

  1. J.-C. Schwartz, G. Barbin, A.-M. Duchemin, M. Garbarg, C. Llorens, H. Pollard, T. T. Quach and C. Rose, Histamine Receptors in the brain and their possible functions. InPharmacology of Histamine Receptors (Eds C. R. Ganellin and M. E. Parsons). Wright·PSG, Bristol, London, Boston 1982.

    Google Scholar 

  2. L. R. Hegstrand, P. D. Kanof and P. Greengard,Histamine-sensitive adenylate cyclase in Mammalian brain. Nature260, 165–167 (1976).

    PubMed  Google Scholar 

  3. P. D. Kanof and P. Greengard,Brain histamine receptors as targets for antidepressant drugs. Nature272, 329–333 (1978).

    PubMed  Google Scholar 

  4. J. P. Green, C. L. Johnson, H. Weinstein and S. Maayani,Antagonism of histamine-activated adenylate cyclase in brain by D. Lysergic acid diethylamide. Proc. Natl. Acad. Sci. USA74, 5697–5701 (1977).

    PubMed  Google Scholar 

  5. J. M. Palacios, M. Garbarg, G. Barbin and J.-C. Schwartz,Pharmacological characterization of histamine receptors mediating the stimulation of cyclic AMP accumulation in slices from guinea-pig hippocampus. Mol. Pharmacol.14, 971–982 (1978).

    PubMed  Google Scholar 

  6. G. A. Gajtkowski D. B. Norris, T. J. Rising and T. P. Wood,Specific binding of 3 H-tiotidine to histamine H 2-receptors in guinea-pig cerebral cortex. Nature304, 65–67 (1983).

    PubMed  Google Scholar 

  7. D. B. Norris, G. A. Gajtkowski and T. J. Rising,Histamine H 2-binding studies in the guinea-pig brain. Agents Actions14, 543–545 (1984).

    PubMed  Google Scholar 

  8. A. DeLean, P. J. Munson and D. Rodbard,Simultaneous analysis of families of sigmoidal curves: application to bioassay, radioligand assay, and physiological dose-response curves. Am. J. Physiol.235, E97-E102 (1978).

    PubMed  Google Scholar 

  9. G. Sperk, H. Hortnagl, H. Reither and O. Hornykiewicz,Evidence for neuronal localization of histamine N-methyl-transferase in rat brain. J. Neurochem.37, 525–526 (1981).

    PubMed  Google Scholar 

  10. W. P. Burkard,Histamine H 2-receptor binding with 3 H-cimetidine in brain. Eur. J. Pharmacol.50, 449–450 (1978).

    PubMed  Google Scholar 

  11. D. A. Kendall, J. W. Ferkany and S. J. Enna,Properties of 3 H-cimetidine binding in rat brain membrane fractions. Life Sci.26, 1293–1302 (1980).

    PubMed  Google Scholar 

  12. I. R. Smith, M. T. Cleverley, C. R. Ganellin and K. M. Metters,Binding of 3 H-cimetidine to rat brain tissue. Agents Actions10, 422–426 (1980).

    PubMed  Google Scholar 

  13. T. J. Rising, D. B. Norris, S. E. Warrander and T. P. Wood,High affinity 3 H-cimetidine binding in guinea-pig tissues. Life Sci.27, 199–206 (1980).

    PubMed  Google Scholar 

  14. S. E. Warrander, D. B. Norris, T. J. Rising and T. P. Wood,3 H-cimetidine and the H 2-receptor. Life Sci.33, 1119–1126 (1983).

    PubMed  Google Scholar 

  15. J. C. Foreman, D. B. Norris T. J. Rising and S. E. Webber,The binding of 3 H-tiotidine to homogenates of guinea-pig lung parenchyma. Br. J. Pharmac.86, 475–482 (1985).

    Google Scholar 

  16. C. R. Ganellin, Chemistry and structure-activity relationships of drugs acting at histamine receptors. InPharmacology of histamine receptors (Eds. C. R. Ganellin and M. E. Parsons) Wright· PSG, Bristol, London, Boston 1982.

    Google Scholar 

Download references

Author information

Affiliations

Authors

Rights and permissions

Reprints and Permissions

About this article

Cite this article

Smith, I.R., Leigh, B.K. & Mylek, M.E. 3H-Tiotidine binding to guinea-pig cortical and striatal membranes. Agents and Actions 19, 169–173 (1986). https://doi.org/10.1007/BF01966202

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF01966202

Keywords

  • Nucleus Accumbens
  • Striatal Membrane
  • Affinity Relationship
  • Affinity Study
  • Suitable Radioligand